(R)‐Propylene carbonate is an important intermediate in the synthesis of tenofovir pro‐drugs such as tenofovir alafenamide fumarate (TAF) and tenofovir diisoproyl fumarate (TDF). Independent of the pro‐drug type, tenofovir presents a chiral secondary hydroxy derivative, which can be obtained directly from (R)‐propylene carbonate. Herein, we report our chemo‐enzymatic continuous‐flow strategy towards (R)‐propylene carbonate starting from a very cheap and renewable raw material, glycerol. We were able to synthesize (R)‐propylene carbonate in seven continuous‐flow steps, starting from glycerol, in good‐to‐excellent yields (66–93 %) and excellent selectivity (E > 200).
Capecitabine
is an important anticancer drug whose synthesis comprises
late-stage carbamoylation and ester hydrolysis. Herein we report the
use of the Schotten–Baumann reaction in order to perform these
transformation in one pot both in batch and under continuous flow.
In batch, capecitabine was obtained in 82% yield in 5 h, while under
continuous flow it was obtained in 81% yield in 30 min. This one-pot
reaction reduces the chemical waste produced, labor, time, and cost
and additionally comprises the use of environmentally friendly solvents
and reagents as well as energy-efficient and safe methods, all of
which fulfill the requirements of a green process.
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